Stable Evans Blue Derived Exendin-4 Peptide for Type 2 Diabetes Treatment

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• 作者：Yi Liu ; Guohao Wang ; Huimin Zhang ; Ying Ma ; Lixin Lang ; Orit Jacobson ; Dale O. Kiesewetter ; Lei Zhu ; Shi Gao ; Qingjie Ma ; Xiaoyuan Chen
• 刊名：Bioconjugate Chemistry
• 出版年：2016
• 出版时间：January 20, 2016
• 年：2016
• 卷：27
• 期：1
• 页码：54-58
• 全文大小：331K
• ISSN：1520-4812

文摘

In the treatment of type 2 diabetes mellitus, it is very important to develop therapeutics with prolonged circulation half-life. Exendin-4 is a glucagon like peptide-1 receptor (GLP-1R) agonist that has been modified in different ways for imaging insulinoma and for treating type-2 diabetes. In this work, we synthesized a maleimide derivative of truncated Evans blue dye (MEB-C3-Mal) to conjugate with (Cys⁴⁰)exendin-4 to obtain a highly stable MEB-C3-(Cys⁴⁰)exendin-4 (denoted as Abextide II). Through in situ binding with endogenous albumin, Abextide II lowers blood glucose level and prolongs the hypoglycemic effect in a type 2 diabetes mouse model more than the FDA approved Albiglutide.